Category: 70931-59-8

On June 7, 2007, Naidu, B. Narasimhulu; Banville, Jacques; Beaulieu, Francis; Connolly, Timothy P.; Krystal, Mark R.; Matiskella, John D.; Ouellet, Carl; Plamondon, Serge; Remillard, Roger; Sorenson, Margaret E.; Ueda, Yasutsugu; Walker, Michael A. published a patent.Computed Properties of 70931-59-8 The title of the patent was Bicyclic heterocycles, particularly 4-oxopyrimido[2,1-c][1,4]oxazine-2-carboxamide and 4-oxopyrimido[2,1-c][1,4]oxazepine-2-carboxamide derivatives, as HIV integrase inhibitors, their preparation, pharmaceutical compositions, and use in therapy. And the patent contained the following:

The invention is related to bicyclic pyrimidinone compounds, e.g. pyrimidooxazine I, which inhibit HIV integrase and prevent viral integration into human DNA. The invention is also related to the preparation of pharmaceutical compositions comprising a therapeutically effective amount of bicyclic pyrimidinones and a pharmaceutically acceptable carrier, optionally including a therapeutically effective amount of at least one other agent used for treatment of AIDS or HIV infection, as well as to the use of the compositions for the treatment of those infected with HIV. Thus, hydrogenolysis of dibenzyl compound II gave phosphonic acid I. I was tested for HIV integrase inhibition and for inhibition of HIV replication. The experimental process involved the reaction of 1-(Bromomethyl)-4-fluoro-2-iodobenzene(cas: 70931-59-8).Computed Properties of 70931-59-8

The Article related to pyrimidinone bicyclic preparation hiv integrase inhibitor, oxopyrimidooxazine oxopyrimidooxazepine carboxamide preparation hiv integrase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Computed Properties of 70931-59-8

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

On February 17, 2009, Naidu, B. Narasimhulu; Sorenson, Margaret E.; Digiugno, Dawn published a patent.Formula: C7H5BrFI The title of the patent was Preparation of bicyclic heterocycles, particularly pyrimido[2,1-c][1,4]oxazine-2-carboxamides, as HIV integrase inhibitors. And the patent contained the following:

The invention is related to the preparation of title compounds I [R1 = C1-6(Ar1)alkyl, C1-6(Ar1)oxyalkyl, C1-6(Ar1)hydroxyalkyl, etc.; R2 = H, alkyl, OH, alkyloxy; Ar1 = (un)substituted Ph, naphthyl, benzothiophenyl, etc.; X-Y-Z = C(R3)2OC(R3)2, C(R3)2OC(R3)2C(R3)2, C(R3)2C(R3)2C(R3)2C(R3)2; R3 = H, alkyl], and their pharmaceutically acceptable salts or solvates which inhibit HIV integrase and prevent viral integration into human DNA. The invention is also related to the pharmaceutical compositions comprising pyrimidinones I, and methods of using them for treating HIV infection and AIDS. Thus, reacting ester II (preparation given) with 4-fluorobenzylamine in DMF/ethanol in the presence of TEA at 90掳 gave amide III in 82% yield. Selected I displayed IC50 values in the range of 0.002-0.1 渭M for the inhibition of HIV integrase activity. III demonstrated synergistic or additive-synergistic HIV antiviral activity when used in combination with other antiviral agents, e.g., zidovudine, indinavir, T-20, etc. Crystalline forms of III were prepared (crystal data were given). The experimental process involved the reaction of 1-(Bromomethyl)-4-fluoro-2-iodobenzene(cas: 70931-59-8).Formula: C7H5BrFI

The Article related to bicyclic heterocycle hiv integrase inhibitor preparation, pyrimidooxazine carboxamide preparation hiv integrase inhibitor aids treatment, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Formula: C7H5BrFI

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

On September 7, 2006, Naidu, B. Narasimhulu; Banville, Jacques; Beaulieu, Francis; Connolly, Timothy P.; Krystal, Mark R.; Matiskella, John D.; Ouellet, Carl; Plamondon, Serge; Remillard, Roger; Sorenson, Margaret E.; Ueda, Yasutsugu; Walker, Michael A. published a patent.Reference of 1-(Bromomethyl)-4-fluoro-2-iodobenzene The title of the patent was Preparation of bicyclic heterocycles, particularly pyrimido[2,1-c][1,4]oxazine-2-carboxamides, as HIV integrase inhibitors. And the patent contained the following:

The invention is related to the preparation of title compounds I [R1 = C1-6(Ar1)alkyl, C1-6(Ar1)oxyalkyl, C1-6(Ar1)hydroxyalkyl, etc.; R2 = H, alkyl, OH, alkyloxy; Ar1 = (un)substituted Ph, naphthyl, benzothiophenyl, etc.; X-Y-Z = C(R3)2OC(R3)2, C(R3)2OC(R3)2C(R3)2, C(R3)2C(R3)2C(R3)2C(R3)2; R3 = H, alkyl], and their pharmaceutically acceptable salts or solvates which inhibit HIV integrase and prevent viral integration into human DNA. The invention is also related to the pharmaceutical compositions comprising pyrimidinones I, and methods of using them for treating HIV infection and AIDS. Thus, reacting ester II (preparation given) with 4-fluorobenzylamine in DMF/ethanol in the presence of TEA at 90掳 gave amide III in 82% yield. Selected I displayed IC50 values in the range of 0.002-0.1 渭M for the inhibition of HIV integrase activity. III demonstrated synergistic or additive-synergistic HIV antiviral activity when used in combination with other antiviral agents, e.g., zidovudine, indinavir, T-20, etc. The experimental process involved the reaction of 1-(Bromomethyl)-4-fluoro-2-iodobenzene(cas: 70931-59-8).Reference of 1-(Bromomethyl)-4-fluoro-2-iodobenzene

The Article related to bicyclic heterocycle hiv integrase inhibitor preparation, pyrimidooxazine carboxamide preparation hiv integrase inhibitor aids treatment, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Reference of 1-(Bromomethyl)-4-fluoro-2-iodobenzene

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

On June 7, 2007, Naidu, Narasimhulu B.; Ueda, Yasutsugu; Connolly, Timothy P. published a patent.Name: 1-(Bromomethyl)-4-fluoro-2-iodobenzene The title of the patent was Preparation of pyrimidine derivatives as HIV integrase inhibitors. And the patent contained the following:

Title compounds I, wherein R1 is arylalkyl, arylamide, arylester, arylhydroxyalkyl or aryloxyalkyl; R2 is H, alkyl, hydroxy or alkoxy; R3 is (un)substituted methyl; R4 is alkyl are prepared as HIV integrase inhibitors. Thus, II was prepared and displayed and HIV-integrase inhibition between 0.002 to 0.10 渭M and an inhibition of HIV replication between 0.003 to 0.10 渭M. Further, I can successfully be employed as prodrugs for treatment of AIDS or HIV infection selected from the group consisting of nucleoside HIV reverse transcriptase inhibitors, non-nucleoside HIV reverse transcriptase inhibitors, HIV protease inhibitors, HIV fusion inhibitors, HIV attachment inhibitors, CCR5 inhibitors, CXCR inhibitors, HIV budding or maturation inhibitors, and HIV integrase inhibitors. The experimental process involved the reaction of 1-(Bromomethyl)-4-fluoro-2-iodobenzene(cas: 70931-59-8).Name: 1-(Bromomethyl)-4-fluoro-2-iodobenzene

The Article related to pyrimidine preparation hiv integrase inhibition human prodrug, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Name: 1-(Bromomethyl)-4-fluoro-2-iodobenzene

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Linsenmeier, Anna M.; Williams, Craig M.; Brase, Stefan published an article in 2013, the title of the article was Photochemical Synthesis of Phenanthridines: Exploring Fluoro and Protected Catechol Substitution.Name: 1-(Bromomethyl)-4-fluoro-2-iodobenzene And the article contains the following content:

Substituted phenanthridines, such as the natural product trispheridine, have been accessed by the practical photochem. cyclization of N-benzylanilines. Functionalities, with a focus on fluoro substituents and protected catechols, are well tolerated on both the A and C rings. The phenanthridines were accessed in good to very good yields (up to 95 %) from iodinated substrates, whereas brominated substrates performed poorly in comparison (0-48 %). The experimental process involved the reaction of 1-(Bromomethyl)-4-fluoro-2-iodobenzene(cas: 70931-59-8).Name: 1-(Bromomethyl)-4-fluoro-2-iodobenzene

The Article related to iodobenzylaniline fluoro protected catechol containing photochem cyclization, phenanthridine preparation, Heterocyclic Compounds (One Hetero Atom): Other Areno- and Diarenopyridines (Acridines, Quinolizines, etc.) and other aspects.Name: 1-(Bromomethyl)-4-fluoro-2-iodobenzene

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

On December 13, 2018, Bartberger, Michael D.; Beck, Hilary Plake; Degraffenreid, Michael R.; Fox, Brian M.; Gonzalez Lopez De Turiso, Felix; Julian, Lisa D.; Kayser, Frank; Medina, Julio C.; Olson, Steven H.; Rew, Yosup; Roveto, Philip M.; Sun, Daqing; Yan, Xuelei published a patent.Electric Literature of 70931-59-8 The title of the patent was Preparation of cis-morpholinone and other compounds as MDM2 inhibitors for the treatment of cancer. And the patent contained the following:

The invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor. The title compounds [I; X = O or S(O)2; R1 = H, C1-6alkyl, (CReRe)nC6-8aryl, (CReRe)nC3-8cycloalkyl, (CReRe)n-3-8 membered heterocycloalkyl, S(O)2C3-8cycloalkyl, C(O)C3-8cycloalkyl, or CRfRa(CReRe)n-Q; Q = (CReRe)nC6-8aryl, (CReRe)n-3-8 membered heterocycloalkyl, (CReRe)n-5-8 membered heteroaryl, (CReRe)nC3-8cycloalkyl, cyano, (CReRe)nOH, CO2H, NReRe, etc.; R2 = H, C1-6alkyl, (CReRe)nC(O)ORe, (CReRe)nNReRe, (CReRe)nC(O)NReRe, (CReRe)nOH, (CReRe)nC(O)H, (CReRe)nC6-8aryl, (CReRe)n-3-8 membered heterocycloalkyl, (CReRe)n-5-8 membered heteroaryl, (CReRe)nCN, -(CReRe)nC(O)5-8 membered heterocycloalkyl, etc.; any heteroaryl or heterocycloalkyl group has one or more heteroatoms independently selected from O, N or S; any cycloalkyl, heterocycloalkyl, heteroaryl or aryl group can be unsubstituted or substituted; R3 = H or C1-6alkyl; R4 = C6-8 aryl or 5-9 membered heteroaryl; R5 = C6-8 aryl or 5-9 membered heteroaryl; R6, R7 = H or C1-6alkyl; Ra = independently H, C1-6alkyl, C2-6alkenyl, (CReRe)nC3-8cycloalkyl, or (CReRe)nC6-8aryl, wherein any cycloalkyl or aryl group can be unsubstituted or substituted; Re, Rf = independently H, C1-6alkyl , or OH; n, m = independently 0-4; provided that R2 and R3 are not both H] or pharmaceutically acceptable salts thereof were prepared These compounds including morpholinone and 2,5,6,8-tetrahydro-3H-imidazo[2,1-c][1,4]oxazine derivatives are inhibitors of MDM2 (oncoprotein) and are useful as therapeutic agents, particularly for the treatment of cancers. Thus, cyclocondensation of rel-(1R,2S)-1,2-bis(4-bromophenyl)-2-(methylamino)ethanol with 2-chloroacetyl chloride gave rel-(5R,6S)-5,6-bis(4-bromophenyl)-4-methylmorpholin-3-one which was treated with sodium bis(trimethylsilyl)amide followed by benzylation with benzyl bromide yo give rel-(2S,5R,6S)-2-benzyl-5,6-bis(4-bromophenyl)-4-methylmorpholin-3-one (II). II and 2-[rel-(2S,5R,6S)-4-benzyl-6-(3-chlorophenyl)-5-(4-chlorophenyl)-3-oxomorpholin-2-yl]acetic acid (III) showed IC50 of 1.96 and 0.0399 渭M, resp., for inhibiting the interaction of GST-hMDM2 and biotinylated-p53 in an homogeneous time-resolved fluorescence assay (HTRF1 assay). The experimental process involved the reaction of 1-(Bromomethyl)-4-fluoro-2-iodobenzene(cas: 70931-59-8).Electric Literature of 70931-59-8

The Article related to mdm2 oncoprotein inhibitor morpholinone tetrahydroimidazooxazine, morpholinone tetrahydroimidazooxazine preparation treatment cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Electric Literature of 70931-59-8

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

On August 28, 2014, Bartberger, Michael D.; Beck, Hilary Plake; Degraffenreid, Michael R.; Fox, Brian M.; Gonzalez Lopez De Turiso, Felix; Julian, Lisa D.; Kayser, Frank; Medina, Julio C.; Olson, Steven H.; Rew, Yosup; Roveto, Philip M.; Sun, Daqing; Yan, Xuelei published a patent.Related Products of 70931-59-8 The title of the patent was Preparation of cis-morpholinone and other compounds as MDM2 inhibitors for the treatment of cancer. And the patent contained the following:

The title compounds [I; X = O or S(O)2; R1 = H, C1-6alkyl, (CReRe)nC6-8aryl, (CReRe)nC3-8cycloalkyl, (CReRe)n-3-8 membered heterocycloalkyl, S(O)2C3-8cycloalkyl, C(O)C3-8cycloalkyl, or CRfRa(CReRe)n-Q; Q = (CReRe)nC6-8aryl, (CReRe)n-3-8 membered heterocycloalkyl, (CReRe)n-5-8 membered heteroaryl, (CReRe)nC3-8cycloalkyl, cyano, (CReRe)nOH, CO2H, NReRe, etc.; R2 = H, C1-6alkyl, (CReRe)nC(O)ORe, (CReRe)nNReRe, (CReRe)nC(O)NReRe, (CReRe)nOH, (CReRe)nC(O)H, (CReRe)nC6-8aryl, (CReRe)n-3-8 membered heterocycloalkyl, (CReRe)n-5-8 membered heteroaryl, (CReRe)nCN, -(CReRe)nC(O)5-8 membered heterocycloalkyl, etc.; any heteroaryl or heterocycloalkyl group has one or more heteroatoms independently selected from O, N or S; any cycloalkyl, heterocycloalkyl, heteroaryl or aryl group can be unsubstituted or substituted; R3 = H or C1-6alkyl; R4 = C6-8 aryl or 5-9 membered heteroaryl; R5 = C6-8 aryl or 5-9 membered heteroaryl; R6, R7 = H or C1-6alkyl; Ra = independently H, C1-6alkyl, C2-6alkenyl, (CReRe)nC3-8cycloalkyl, or (CReRe)nC6-8aryl, wherein any cycloalkyl or aryl group can be unsubstituted or substituted; Re, Rf = independently H, C1-6alkyl , or OH; n, m = independently 0-4; provided that R2 and R3 are not both H] or pharmaceutically acceptable salts thereof were prepared These compounds including morpholinone and 2,5,6,8-tetrahydro-3H-imidazo[2,1-c][1,4]oxazine derivatives are inhibitors of MDM2 (oncoprotein) and are useful as therapeutic agents, particularly for the treatment of cancers. The cancer is selected from bladder, breast, colon, rectum, kidney, liver, small cell lung cancer, non-small-cell lung cancer, esophagus, gall bladder, ovary, pancreas, stomach, cervix, thyroid, prostate, skin, acute lymphocytic leukemia, chronic myelogenous leukemia, acute lymphoblastic leukemia, B-cell lymphoma, T-cell lymphoma, Hodgkin’s lymphoma, non-Hodgkin’s lymphoma, hairy cell lymphoma, Burkitt’s lymphoma, acute and chronic myelogenous leukemia, melanoma, endometrial cancer, head and neck cancer, glioblastoma, or osteosarcoma. Thus, cyclocondensation of rel-(1R,2S)-1,2-bis(4-bromophenyl)-2-(methylamino)ethanol with 2-chloroacetyl chloride in the presence of Et3N in THF at 0掳 for 1 h gave rel-(5R,6S)-5,6-Bis(4-bromophenyl)-4-methylmorpholin-3-one which was treated with sodium bis(trimethylsilyl)amide in THF at -78掳 for 20 min and then underwent benzylation with benzyl bromide at -78掳 for 30 min and at room temperature for 30 min to give rel-(2S,5R,6S)-2-benzyl-5,6-bis(4-bromophenyl)-4-methylmorpholin-3-one (II). II and 2-[rel-(2S,5R,6S)-4-benzyl-6-(3-chlorophenyl)-5-(4-chlorophenyl)-3-oxomorpholin-2-yl]acetic acid (III) showed IC50 of 1.96 and 0.0399 渭M, resp., for inhibiting the interaction of GST-hMDM2 and biotinylated-p53 in an homogeneous time-resolved fluorescence assay (HTRF1 assay). The experimental process involved the reaction of 1-(Bromomethyl)-4-fluoro-2-iodobenzene(cas: 70931-59-8).Related Products of 70931-59-8

The Article related to mdm2 oncoprotein inhibitor morpholinone tetrahydroimidazooxazine, morpholinone tetrahydroimidazooxazine preparation treatment cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Related Products of 70931-59-8

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

On September 5, 2012, Zhou, Fengtao; Guo, Jiajia; Liu, Jianguang; Ding, Ke; Yu, Shouyun; Cai, Qian published an article.Recommanded Product: 70931-59-8 The title of the article was Copper-Catalyzed Desymmetric Intramolecular Ullmann C-N Coupling: An Enantioselective Preparation of Indolines. And the article contained the following:

The first highly enantioselective copper-catalyzed intramol. Ullmann C-N coupling reaction has been developed. The asym. desymmetrization of 1,3-bis(2-iodoaryl)propan-2-amines catalyzed by CuI/(R)-BINOL-derived ligands led to the enantioselective formation of indolines in high yields and excellent enantiomeric excesses. This method was also applied to the formation of 1,2,3,4-tetrahydroquinolines in high yields and excellent enantioselectivity. The experimental process involved the reaction of 1-(Bromomethyl)-4-fluoro-2-iodobenzene(cas: 70931-59-8).Recommanded Product: 70931-59-8

The Article related to iodoarylpropanamine iodoarylpentanamine copper binol catalyzed desymmetrization intramol ullmann coupling, indoline tetrahydroquinoline stereoselective preparation, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Recommanded Product: 70931-59-8

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

On July 31, 2003, Egbertson, Melissa; Melamed, Jeffrey Y.; Langford, H. Marie; Young, Steven D. published a patent.Application In Synthesis of 1-(Bromomethyl)-4-fluoro-2-iodobenzene The title of the patent was Preparation of hydroxynaphthyridinone carboxamides useful as HIV integrase inhibitors. And the patent contained the following:

Hydroxynaphthyridinone carboxamides (shown as I; variables defined below; e.g. N-(4-fluorobenzyl)-4-hydroxy-2-oxo-1,2-dihydro-1,5-naphthyridine-3-carboxamide) are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds were employed against HIV infection and AIDS as compounds per se or as pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions (one example given), optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described. Although the methods of preparation are not claimed, 27 example preparations of I are included; all have IC50’s <0.5 渭M in a HIV integrase assay and all have IC95's <5 渭M in an assay for inhibition of HIV replication. For I: L = linker connecting the C atom of the Ph ring to the N of the -NH- moiety = single bond, -(C1-6 alkyl)- (un)substituted with -C(O)N(RaRb), -(C0-3 alkyl)-C:C-(C1-3-alkyl)-, -(C0-3 alkyl)-C顚咰-(C1-3-alkyl)-, or -(C0-6 alkyl)-(C3-6 cycloalkyl)-(C0-6-alkyl)-. R1a, R1b, and R1c = H, halogen, -C1-6 alkyl, or -C1-6 haloalkyl; R2a and R2b = H, -C1-6 (un)substituted alkyl, -O-C1-6 (un)substituted alkyl, -OH, halo, -NO2, -CN, -C(O)Ra, -CO2Ra, -S(O)nRa, -SO2N(RaRb), -N(RaRb), -C(O)N(RaRb), -N(Ra)SO2Rb, -OC(O)N(RaRb), -N(Ra)C(O)N(RaRb), -N(Ra)-C1-6-alkyl-C(O)N(RaRb), -N(Ra)-C(O)-C1-6 alkyl-N(RaRb), -N(Ra)C(O)-C(O)N(RaRb), -OCO2Ra, -N(Ra)-SO2N(RaRb), -N(Ra)-SO2-C1-6 alkyl-N(RaRb), -N(Ra)C(O)Rb, -N(Ra)CO2Rb, -S-C1-6 alkyl-C(O)N(RaRb),or -N(SO2Ra)-C1-6 alkyl-C(O)N(RaRb). R3 = H, -C1-6-(un)substituted alkyl, -S(O)nRa, -SO2N(RaRb), -C2-6 (un)substituted alkenyl, -C2-5 (un)substituted alkynyl, -Rk, -S(O)n-C1-6 alkyl-Rk, -N(Ra)C(O)-Rk, or -N(Ra)C(O)-C1-6 alkyl-Rk; each of R4 and R5 = H, -C1-6 (un)substituted alkyl, -SO2N(RaRb), or -C1-6 alkyl-Rm; each Ra and Rb = H, -C1-6 alkyl, or -C3-8 cycloalkyl; Rk is a carbocycle or a heterocycle; each Rm = a carbocycle or a heterocycle; each n = 0, 1 or 2; addnl. details including provisos are given in the claims. The experimental process involved the reaction of 1-(Bromomethyl)-4-fluoro-2-iodobenzene(cas: 70931-59-8).Application In Synthesis of 1-(Bromomethyl)-4-fluoro-2-iodobenzene

The Article related to hydroxynaphthyridinone carboxamide preparation hiv integrase inhibitor, aids drug hydroxynaphthyridinone carboxamide preparation hiv integrase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.Application In Synthesis of 1-(Bromomethyl)-4-fluoro-2-iodobenzene

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Liu, Can; Zhu, Xianjin; Han, Yongzhen; Yang, Haijun; Zhu, Changjin; Fu, Hua published an article in 2019, the title of the article was Superbase-promoted selective carbon-carbon bond cleavage driven by aromatization.Application of 70931-59-8 And the article contains the following content:

A novel selective carbon-carbon single bond cleavage has been disclosed through the copper-catalyzed reaction of 1-alkyl-3-alkylindolin-2-imine hydrochlorides I鈥Cl (R1 = 7-CH3, 5-OCH3, 5-Cl, etc.; R2 = CH3, CH2C6H5, CH2CH=CH2, etc.; R3 = C2H5, CH2C6H5, 4-ClC6H4CH2, etc.) with substituted 1-(bromomethyl)-2-iodobenzenes R4-2-(X)C6H3CH2Br (R4 = H, 5-OCH3, 4-F, 5-F, 5-Cl; X = I, Br) leading to fused N-heterocycles II (R5 = 7-CH3, 9-OCH3, 9-Cl, etc.; R6 = 2-OCH3, 3-F, 2-F, 2-Cl). Mechanistic studies showed that the intrinsic drive of aromatization and the action of the superbase derived from sodium tert-butoxide and dimethylsulfoxide were the key factors leading to the carbon-carbon single bond cleavage. Furthermore, the obtained N-heterocycles are indoloquinoline derivatives II with wide biol. activities. The experimental process involved the reaction of 1-(Bromomethyl)-4-fluoro-2-iodobenzene(cas: 70931-59-8).Application of 70931-59-8

The Article related to indoloquinoline preparation chemoselective, alkyl alkylindolin imine hydrochloride bromomethyl iodobenzene aromatization copper catalyst, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.Application of 70931-59-8

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com